Alestramustine
Alestramustine.svg | |
Alestramustine (INN ), also known as estradiol 3-(bis(2-chloroethyl)carbamate) 17β-(L-alaninate), is a cytostatic antineoplastic agent which was never marketed.[1][2] It is the L-alanine ester of estramustine, which is a combination of the nitrogen mustard normustine coupled via a carbamate to the estrogen estradiol.[1][3] Alestramustine acts as a prodrug to estramustine, and also forms estradiol as a byproduct.[1][3] The drug, via its active metabolites, binds to microtubule-associated proteins and β-tubulin and interferes with microtubule function, thereby inhibiting cell division.[1][3] Due to its estrogen moiety, alestramustine is selectively concentrated in estrogen receptor-positive cells such as prostate and breast.[1]
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Contributors: Prab R. Tumpati, MD